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Preparation and characterization of biodegradable polyhydroxybutyrate-co-hydroxyvalerate/polyethylene glycol-based microspheres
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Alexandre Monnier, Charlotte Rombouts, Dania Kouider, Imad About, Hatem Fessi, Nida Sheibat-Othman The in vivo effectiveness of biomolecules may be limited by their rapid diffusion in the body and short half-life time. Encapsulation of these biomolecules allows protecting them against degradation and ensuring a controlled release over time. In this work, the production of polyhydroxybutyrate-co-hydroxyvalerate/polyethylene glycol-based microspheres loaded with heparin by double emulsion-solvent evapora...
Source: International Journal of Pharmaceutics - September 7, 2016 Category: Drugs & Pharmacology Source Type: research

Arginine as a protein stabilizer and destabilizer in liquid formulations
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Nam Ah Kim, Sharvron Hada, Ritu Thapa, Seong Hoon Jeong Even though arginine monohydrochloride (ArgHCl) is a useful additive for protein stabilization, its mechanism is not yet fully elucidated. Moreover, there is a concern that ArgHCl may be a protein denaturant since it decreases transition melting temperature (Tm ) of certain proteins. It contains a guanidinium group, a critical structure for denaturating activity of guanidine hydrochloride (GndHCl). Effects of ArgHCl, GndHCl, and creatinine on a mo...
Source: International Journal of Pharmaceutics - September 7, 2016 Category: Drugs & Pharmacology Source Type: research

Near infrared spectroscopy to monitor drug release in-situ during dissolution tests
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Mafalda Cruz Sarraguça, Rita Matias, Raquel Figueiredo, Paulo Roberto S. Ribeiro, Ana Teixeira Martins, João Almeida Lopes Dissolution tests can be used to demonstrate suitable in vivo drug release through in vivo/in vitro correlations. This work explores the possibility of using near infrared spectroscopy (NIRS) to monitor in-situ dissolution tests. It aims at expanding surrogate methods in quality control of drug products. Laboratory designed tablets of an immediate-release formulation ...
Source: International Journal of Pharmaceutics - September 6, 2016 Category: Drugs & Pharmacology Source Type: research

When food can make the difference: The case of elvitegravir-based co-formulation
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Dario Cattaneo, Sara Baldelli, Davide Minisci, Paola Meraviglia, Emilio Clementi, Massimo Galli, Cristina Gervasoni Stribild should be administered under fed conditions to optimize drugs exposure. Here we assessed to what extent this advice is applied in the real life scenario by therapeutic drug monitoring in 75 HIV-infected patients given Stribild-based antiretroviral therapy. Fifty-three percent of our patients took Stribild at lunch/supper time, 23% in the morning with breakfast, and 24% middle in the mornin...
Source: International Journal of Pharmaceutics - September 3, 2016 Category: Drugs & Pharmacology Source Type: research

Solubilization and formulation of chrysosplenol C in solid dispersion with hydrophilic carriers
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Choon Lian Ng, Sang-Eun Lee, Joon-Kyung Lee, Tae-Hyeon Kim, Woo Suk Jang, Jin-Seok Choi, Young-Ho Kim, Jin-Ki Kim, Jeong-Sook Park We investigated how to overcome problems associated with the solubility, dissolution, and oral bioavailability of the poorly water-soluble drug compound, chrysosplenol C (CRSP), as well as the effects of single and binary hydrophilic polymers (PVP K-25 and/or PEG 6000) on the solubility and dissolution parameters of CRSP. Then an optimized formulation was further developed with a sur...
Source: International Journal of Pharmaceutics - September 3, 2016 Category: Drugs & Pharmacology Source Type: research

Nanocomposite microparticles (nCmP) for the delivery of tacrolimus in the treatment of pulmonary arterial hypertension
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Zimeng Wang, Julie L. Cuddigan, Sweta K. Gupta, Samantha A. Meenach Tacrolimus (TAC) has exhibited promising therapeutic potential in the treatment of pulmonary arterial hypertension (PAH); however, its application is prevented by its poor solubility, instability, poor bioavailability, and negative systemic side effects. To overcome the obstacles of using TAC for the treatment of PAH, we developed nanocomposite microparticles (nCmP) for the pulmonary delivery of tacrolimus in the form of dry powder aerosols. The...
Source: International Journal of Pharmaceutics - September 3, 2016 Category: Drugs & Pharmacology Source Type: research

Solid lipid nanoparticles co-loaded with doxorubicin and α-tocopherol succinate are effective against drug-resistant cancer cells in monolayer and 3-D spheroid cancer cell models
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Mariana S. Oliveira, Bhawani Aryasomayajula, Bhushan Pattni, Samuel V. Mussi, Lucas A.M. Ferreira, Vladmir P. Torchilin This work aimed to develop solid lipid nanoparticles (SLN) co-loaded with doxorubicin and α-tocopherol succinate (TS) and to evaluate its potential to overcome drug resistance and to increase antitumoral effect in MCF-7/Adr and NCI/Adr cancer cell lines. The SLN were prepared by a hot homogenization method and characterized for size, zeta potential, entrapment efficiency (EE), and drug lo...
Source: International Journal of Pharmaceutics - September 3, 2016 Category: Drugs & Pharmacology Source Type: research

In-vivo disposition characteristics of PEG niosome and its interaction with serum proteins
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Tamer Shehata, Toshikiro Kimura, Kazutaka Higaki, Ken-ichi Ogawara Three different nonionic surfactants (Brij 72, Span 20 and Tween 60) were used to prepare various naked and PEG niosomes. In-vivo study demonstrated that PEGylation dramatically increased the AUC and decreased the affinity to the liver of Brij 72 and Span 20 niosomes in rats. Liver perfusion experiments suggested that the hepatic uptake of naked Brij 72 and Span 20 niosomes could mainly be ascribed to the receptor-mediated uptake, while PEGylatio...
Source: International Journal of Pharmaceutics - September 3, 2016 Category: Drugs & Pharmacology Source Type: research

Exploring the effect of hydrophilic and hydrophobic structure of grafted polymeric micelles on drug loading
The objective of this paper is to explore the effect of hydrophilic and hydrophobic structure of grafted polymeric micelles on drug loading, and elucidate whether drug-polymer compatibility, as predicted by Hansen solubility parameters (HSPs), can be used as a tool for drug-polymer pairs screening and guide the design of grafted polymeric micelles. HSPs of 27 drugs and three grafted copolymers were calculated according to group contribution method. The drug-polymer compatibilities were evaluated using the approaches of Flory-Huggins interaction parameters (χFH) and polarity difference (△Xp). Two models, model A and B...
Source: International Journal of Pharmaceutics - September 1, 2016 Category: Drugs & Pharmacology Source Type: research

Vitamin E TPGS modified liposomes enhance cellular uptake and targeted delivery of luteolin: An in vivo/in vitro evaluation
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Jinli Li, Xudong Cheng, Yan Chen, Weiming He, Li Ni, Peihua Xiong, Minggang Wei Luteolin (LUT) is an active agent in cancer prevention and a potential candidate for clinical chemotherapy. However, poor water solubility and extensive excretion have limited the clinical use of luteolin. Herein, we attempted to develop vitamin E d-α-tocopherol acid polyethylene glycol 1000 succinate (TPGS) coated liposomes to improve the accumulation of luteolin in lung cancer. Luteolin or coumarin-6 loaded liposomes were pre...
Source: International Journal of Pharmaceutics - September 1, 2016 Category: Drugs & Pharmacology Source Type: research

Supramolecular assistance between cyclodextrins and didecyldimethylammonium chloride against enveloped viruses: Toward eco-biocidal formulations
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Loïc Leclercq, Anny Dewilde, Jean-Marie Aubry, Véronique Nardello-Rataj Nosocomial infections have emerged as important causes of morbidity and mortality in immunocompromised individuals. In this respect, biocides are widely used in hospitals leading to resistant microorganisms. We show here that cyclodextrins can remarkably boost the virucidal activity of di-n-decyldimethylammonium chloride. These oligosaccharides synergistically work with the biocide affording a noticeable reduction of the active v...
Source: International Journal of Pharmaceutics - September 1, 2016 Category: Drugs & Pharmacology Source Type: research

CombiCap: A novel drug formulation for the basel phenotyping cocktail
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Marine Camblin, Benjamin Berger, Manuel Haschke, Stephan Krähenbühl, Jörg Huwyler, Maxim Puchkov Phenotyping of cytochrome P450 isoenzymes is used for metabolic profiling. Phenotyping cocktails are usually administered as individual marketed products, which are not designed for diagnostic applications. Therefore, a formulation strategy was developed, which can be applied to any phenotyping cocktail. The formulation was validated in vitro and in vivo in human volunteers using caffeine, efavirenz, f...
Source: International Journal of Pharmaceutics - August 31, 2016 Category: Drugs & Pharmacology Source Type: research

A design space exploration for control of Critical Quality Attributes of mAb
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Hemlata Bhatia, Erik Read, Cyrus Agarabi, Kurt Brorson, Scott Lute, Seongkyu Yoon A unique “design space (DSp) exploration strategy,” defined as a function of four key scenarios, was successfully integrated and validated to enhance the DSp building exercise, by increasing the accuracy of analyses and interpretation of processed data. The four key scenarios, defining the strategy, were based on cumulative analyses of individual models developed for the Critical Quality Attributes (23 Glycan Profiles) ...
Source: International Journal of Pharmaceutics - August 29, 2016 Category: Drugs & Pharmacology Source Type: research

Synthesis and physicochemical properties of polyacrylamide nanoparticles as photosensitizer carriers
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): M.S. Gualdesi, C.I. Alvarez Igarzabal, J. Vara, C.S. Ortiz At present, polyacrylamide nanoparticles are attractive to drug delivery. However, some physicochemical characteristics of these nanoparticles still need to be further improved in practice. Polyacrylamide nanoparticles with an average size of 80nm and a zeta potential of −30mV were synthesized and used as photosensitizer carriers. The new monobrominated derivatives and parent compounds were the photosensitizers for the photodynamic therapy loaded i...
Source: International Journal of Pharmaceutics - August 29, 2016 Category: Drugs & Pharmacology Source Type: research

Rationally designed particle preloading method to improve protein delivery performance of electrospun polyester nanofibers
This study aimed to improve the protein delivery performance of polyester nanofibers by rationally designing a particle preloading method. Positively charged chitosan nanoparticles (CNPs) were used as carriers to adsorb negatively charged proteins in mild conditions and as primary barriers for protein release. The polar CNPs were then homogeneously dispersed in a polar polyester solution and subjected to electrospinning. Microscope observations indicated that CNPs were homogeneously embedded within polyester nanofibers. In vitro release behaviour and cell studies showed that proteins retained their bioactivity and could re...
Source: International Journal of Pharmaceutics - August 29, 2016 Category: Drugs & Pharmacology Source Type: research

Improved oral bioavailability and anticancer efficacy on breast cancer of paclitaxel via Novel Soluplus ®—Solutol® HS15 binary mixed micelles system
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Jian Hou, E. Sun, Congyong Sun, Jing Wang, Lei Yang, Xiao-bin Jia, Zhen-hai Zhang The aim of this study was to develop a novel drug delivery system using two biocompatible copolymers of Solutol®HS15 and Soluplus® to improve solubility, oral bioavailability and anticancer activity of paclitaxel (PTX). The PTX-loaded mixed micelles (PTX-M) were prepared by ethanol thin-film hydration method. The optimal PTX-M were provided with small size (164.8±2.0nm) and spherical shape at ratio of 1: 3 (Solutol&r...
Source: International Journal of Pharmaceutics - August 29, 2016 Category: Drugs & Pharmacology Source Type: research

Fabrication of magnetite nano particles and modification with metal organic framework of Zn2+ for sorption of doxycyline
This study presents a novel method for synthesis and characterization of a metal-organic framework and application in drug delivery. The first step was synthesis of amino functionalized magnetite that was then modified by a metal-organic framework of Zn2+. This newly developed nano-sorbent was characterized by Fourier transform infrared spectroscopy, scanning electron microscopy, energy dispersive x-ray spectroscopy, thermogravimetric analysis, vibrating sample magnetometer and x-ray diffraction. Doxycycline was loaded to the nano-sorbent and effects of the variable parameters, kinetics of adsorption, release and capacity ...
Source: International Journal of Pharmaceutics - August 29, 2016 Category: Drugs & Pharmacology Source Type: research

Comparative evaluation of rivastigmine permeation from a transdermal system in the Franz cell using synthetic membranes and pig ear skin with in vivo-in vitro correlation
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Alice Simon, Maria Inês Amaro, Anne Marie Healy, Lucio Mendes Cabral, Valeria Pereira de Sousa In the present study, in vitro permeation experiments in a Franz diffusion cell were performed using different synthetic polymeric membranes and pig ear skin to evaluate a rivastigmine (RV) transdermal drug delivery system. In vitro-in vivo correlations (IVIVC) were examined to determine the best model membrane. In vitro permeation studies across different synthetic membranes and skin were performed for the Exelo...
Source: International Journal of Pharmaceutics - August 29, 2016 Category: Drugs & Pharmacology Source Type: research

The development of a growth regime map for a novel reverse-phase wet granulation process
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Jonathan B. Wade, Gary P. Martin, David F. Long The feasibility of a novel reverse-phase wet granulation process has been established and potential advantages identified. Granule growth in the reverse-phase process proceeds via a steady state growth mechanism controlled by capillary forces, whereas granule growth in the conventional process proceeds via an induction growth regime controlled by viscous forces. The resultant reverse-phase granules generally have greater mass mean diameter and lower intragranular p...
Source: International Journal of Pharmaceutics - August 29, 2016 Category: Drugs & Pharmacology Source Type: research

Imaging of in vitro parenteral drug precipitation
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Daniel C. Evans, Michael W. Kudenov, Kimberly C. Sassenrath, Eustace L. Dereniak, Samuel H. Yalkowsky Solid particulate matter introduced into the bloodstream as a result of parenteral drug administration can produce serious pathological conditions. Particulate matter that cannot be eliminated by pre-infusion filtration is often the result of drug precipitation that occurs when certain parenteral formulations are mixed with blood. A new device is designed to model the mixing of drug formulations with flowing blo...
Source: International Journal of Pharmaceutics - August 29, 2016 Category: Drugs & Pharmacology Source Type: research

Dual-acting, function-responsive, and high drug payload nanospheres for combining simplicity and efficacy in both self-targeted multi-drug co-delivery and synergistic anticancer effect
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Yang Li, Jinyan Lin, Guihua Liu, Jinyuan Ma, Liya Xie, Fuqiang Guo, Xuan Zhu, Zhenqing Hou Recently, the global trend in the field of nanomedicine has been toward the design of highly sophisticated drug delivery systems with specific targeting and synergistic therapeutic functions for improving therapeutic efficacy. But offering sophistication generally increases their complexity that might be disadvantageous in pharmaceutical development. We hypothesize that using a macromolecular prodrug with a dual role will ...
Source: International Journal of Pharmaceutics - August 29, 2016 Category: Drugs & Pharmacology Source Type: research

Effect of different polymers on avanafil –β-cyclodextrin inclusion complex: in vitro and in vivo evaluation
In this study, we examined the effect of different polymers on the chemical, physical and pharmacokinetic properties of avanafil–β-cyclodextrin (β-CD) inclusion complex. Equimolar mixtures of drug and β-CD were used to prepare 25 ternary drug–β-CD-polymer inclusion complexes using five different polymers, polyethylene glycol (PEG 4000), polyvinyl pyrrolidone (PVP K-30), chitosan, hydroxypropylmethyl cellulose, and hydroxyethyl cellulose, each in five different concentrations, 1, 3, 5, 7, and 10% (w/w). The addition of 10% (w/w) PEG 4000 resulted in a significant decrease of drug solubility, ...
Source: International Journal of Pharmaceutics - August 29, 2016 Category: Drugs & Pharmacology Source Type: research

Stearic acid and high molecular weight PEO as matrix for the highly water soluble metoprolol tartrate in continuous twin-screw melt granulation
This study aims to investigate the continuous twin screw melt granulation technique to study the impact of a SA/PEO matrix on the dissolution rate of a highly water soluble drug (MPT). Decreasing the SA/PEO ratio improved the release-sustaining properties of the matrix. The solid state of the granules was characterized using differential scanning calorimetry (DSC), nuclear magnetic resonance (NMR), X-ray diffraction (XRD), Raman spectroscopy, Fourier transform infrared (FTIR) and near infrared chemical imaging (NIR-CI) in order to understand the dissolution behavior. The results revealed a preferential interaction of the M...
Source: International Journal of Pharmaceutics - August 29, 2016 Category: Drugs & Pharmacology Source Type: research

Degradation of acetalated dextran can be broadly tuned based on cyclic acetal coverage and molecular weight
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Naihan Chen, Michael A. Collier, Matthew D. Gallovic, Graham C. Collins, Carla C. Sanchez, Elizabeth Q. Fernandes, Eric M. Bachelder, Kristy M. Ainslie Microparticles (MPs) derived from acid-sensitive biopolymers enable rapid degradation and cargo release under acidic conditions, such as at tumor microenvironments, within lysosomal/phagosomal compartments inside phagocytic cells, or at sites of inflammation. One such acid-sensitive biopolymer, acetalated dextran (Ace-DEX), has tunable degradation rates and pH-ne...
Source: International Journal of Pharmaceutics - August 28, 2016 Category: Drugs & Pharmacology Source Type: research

Cardiovascular safety pharmacology studies in dogs enabled for a poorly soluble molecule using spray-dried dispersion: Impact on lead selection
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Yin-Chao Tseng, Brian Linehan, Khing Jow Ng, Dustin M. Smith, Michael Markert, Mita Patel, Brian Guth, Ryan M. Fryer The aim of this study was to identify an adequate formulation for a poorly soluble lead molecule (BI-A) that would achieve sufficiently high plasma concentrations after oral administration in dogs to enable a robust cardiovascular safety pharmacology assessment in telemetry-instrumented conscious dogs during lead optimization in drug discovery. A spray-dried dispersion of BI-A (BI-A-SDD) containin...
Source: International Journal of Pharmaceutics - August 28, 2016 Category: Drugs & Pharmacology Source Type: research

Development of microparticles for oral administration of the non-conventional radical scavenger IAC and testing in an inflammatory rat model
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Nadia Passerini, Beatrice Albertini, Marcello Di Sabatino, Giuseppe Corace, Barbara Luppi, Donatella Canistro, Fabio Vivarelli, Silvia Cirillo, Antonio Soleti, Giulia Merizzi, Moreno Paolini The bis (1-hydroxy-2,2,6,6-tetramethyl-4-piperidinyl)-decandioate (IAC), is an innovative non- radical scavenger used with success in numerous disease models such as inflammation, neurological disorders, hepatitis and diabetes. The pharmacological treatments have been performed by the intraperitoneal route of administration,...
Source: International Journal of Pharmaceutics - August 28, 2016 Category: Drugs & Pharmacology Source Type: research

Enhanced oral delivery of celecoxib via the development of a supersaturable amorphous formulation utilising mesoporous silica and co-loaded HPMCAS
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): A.-L. Lainé, D. Price, J. Davis, D. Roberts, R. Hudson, K. Back, P. Bungay, N. Flanagan Stabilization of amorphous formulations via mesoporous silica has gained considerable attention for oral delivery of poorly soluble drugs. The release of the drug from the silica is expected to generate supersaturation which is often associated with subsequent precipitation. The aim of the study was hence to develop a novel supersaturable amorphous formulation through the co-loading of a BCS class II drug Celecoxib (CX...
Source: International Journal of Pharmaceutics - August 26, 2016 Category: Drugs & Pharmacology Source Type: research

Delivery of Copper-chelating Trientine (TETA) to the central nervous system by surface modified liposomes
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Robin Tremmel, Philipp Uhl, Frieder Helm, Dominik Wupperfeld, Max Sauter, Walter Mier, Wolfgang Stremmel, Götz Hofhaus, Gert Fricker The existence of the blood-brain barrier (BBB) complicates the treatment of many central nervous system (CNS) disorders, including the copper storage disease, Wilson’s disease. Its CNS symptoms represent a serious problem, since therapeutics for Wilson’s disease do not cross the BBB. One strategy to overcome this obstacle is the transfer of drugs across the BBB wit...
Source: International Journal of Pharmaceutics - August 24, 2016 Category: Drugs & Pharmacology Source Type: research

Development of polymeric irinotecan nanoparticles using a novel lactone preservation strategy
In this study, we developed polymeric nanoparticles (NPs) that not only deliver IRT to tumor sites, but also overcome its drawbacks by preserving active lactone conformation, prolonging the plasma circulation time, and by providing sustained release. IRT complex was rendered hydrophobic by ion-pairing with anions (docusate sodium, sodium lauryl sulfate, and sodium tripolyphosphate), and loaded in PEG-PLGA NPs via water/oil/water double emulsification method. The NPs were spherical, ∼60nm, monodispersed, and had shell-core morphology. They retained >80% lactone form for more than 1 month of storage and exh...
Source: International Journal of Pharmaceutics - August 24, 2016 Category: Drugs & Pharmacology Source Type: research

Saturated fatty acids and fatty acid esters promote the polymorphic transition of clarithromycin metastable form I crystal
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Miteki Watanabe, Midori Mizoguchi, Hajime Aoki, Yasunori Iwao, Shuji Noguchi, Shigeru Itai The phase transition of active pharmaceutical ingredients should be taken into account during manufacturing, processing- and storage, because different crystal forms lead to different physical properties of formulations. The phase transition of clarithromycin (CAM) metastable form I to stable form II was investigated on heating with additives such as fatty acids or fatty acid esters. Differential scanning calorimetry analy...
Source: International Journal of Pharmaceutics - August 24, 2016 Category: Drugs & Pharmacology Source Type: research

Enabling real time release testing by NIR prediction of dissolution of tablets made by continuous direct compression (CDC)
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Pallavi Pawar, Yifan Wang, Golshid Keyvan, Gerardo Callegari, Alberto Cuitino, Fernando Muzzio A method for predicting dissolution profiles of directly compressed tablets for a fixed sustained release formulation manufactured in a continuous direct compaction (CDC) system is presented. The methodology enables real-time release testing (RTRt). Tablets were made at a target drug concentration of 9% Acetaminophen, containing 90% lactose and 1% Magnesium Stearate, and at a target compression force of 24kN. A model f...
Source: International Journal of Pharmaceutics - August 24, 2016 Category: Drugs & Pharmacology Source Type: research

Integrating a novel SN38 prodrug into the PEGylated liposomal system as a robust platform for efficient cancer therapy in solid tumors
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Tao Fang, Yuehan Dong, Xiaomin Zhang, Ke Xie, Li Lin, Hangxiang Wang Liposomal nanoassemblies have been used extensively as carriers for the delivery of both lipophilic and hydrophilic drugs. They represent a mature, versatile technology with considerable potential for improving the pharmacokinetics of drugs. However, the formulation of many chemotherapeutics into liposome systems has posed a significant challenge due to their incompatible physicochemical properties, as was the case with camptothecin-based chemo...
Source: International Journal of Pharmaceutics - August 23, 2016 Category: Drugs & Pharmacology Source Type: research

Adhesion of thiolated silica nanoparticles to urinary bladder mucosa: Effects of PEGylation, thiol content and particle size
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Ellina A. Mun, Adrian C. Williams, Vitaliy V. Khutoryanskiy Intravesical drug administration is used to deliver cytotoxic agents through a catheter to treat bladder cancer. One major limitation of this approach is poor retention of the drug in the bladder due to periodic urine voiding. Mucoadhesive dosage forms thus offer significant potential to improve drug retention in the bladder. Here, we investigate thiolated silica nanoparticles retention on porcine bladder mucosa in vitro, quantified through Wash Out50 (...
Source: International Journal of Pharmaceutics - August 23, 2016 Category: Drugs & Pharmacology Source Type: research

( −)-Epigallocatechin gallate (EGCG)-nanoethosomes as a transdermal delivery system for docetaxel to treat implanted human melanoma cell tumors in mice
The objective of this study was to develop EGCG-nanoethosomes for transdermal delivery and to evaluate them for treating subcutaneously implanted human melanoma cell tumors. EGCG-nanoethosomes, composed of 0.2% EGCG, 2% soybean phosphatidylcholine, 30% ethanol, 1% Tween-80 and 0.1% sugar esters, were prepared and characterized using laser transmission electron microscopy. These nanoethosomes were smoother and more compact than basic-nanoethosomes with the same components except for EGCG. The effectiveness of transdermal delivery by EGCG-nanoethosomes was demonstrated in an in vitro permeability assay system using mouse ski...
Source: International Journal of Pharmaceutics - August 23, 2016 Category: Drugs & Pharmacology Source Type: research

Near infrared spectroscopic calibration models for real time monitoring of powder density
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Andrés D. Román-Ospino, Ravendra Singh, Marianthi Ierapetritou, Rohit Ramachandran, Rafael Méndez, Carlos Ortega-Zuñiga, Fernando J. Muzzio, Rodolfo J. Romañach Near infrared spectroscopic (NIRS) calibration models for real time prediction of powder density (tap, bulk and consolidated) were developed for a pharmaceutical formulation. Powder density is a critical property in the manufacturing of solid oral dosages, related to critical quality attributes such as tablet mass, hard...
Source: International Journal of Pharmaceutics - August 23, 2016 Category: Drugs & Pharmacology Source Type: research

Circumvention of P-gp and MRP2 mediated efflux of lopinavir by a histidine based dipeptide prodrug
Conclusion Histidine based dipeptide prodrug approach can be an alternative strategy to improve LPV absorption across poorly permeable intestinal barrier. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 23, 2016 Category: Drugs & Pharmacology Source Type: research

Methotrexate loaded lipid nanoparticles for topical management of skin-related diseases: Design, characterization and skin permeation potential
Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Mara Ferreira, Elisabete Silva, Luísa Barreiros, Marcela A. Segundo, Sofia A. Costa Lima, Salette Reis Methotrexate exhibits poor cutaneous bioavailability when administered topically using conventional vehicles. It is recommended for the treatment of skin-related diseases but its systemic side effects hamper application. The aim of this work was to formulate methotrexate in nanostructured lipid carriers using biocompatible lipids, and to investigate their potential for topical drug delivery. Methotrexate...
Source: International Journal of Pharmaceutics - August 20, 2016 Category: Drugs & Pharmacology Source Type: research

In vivo behavior of MIL-100 nanoparticles at early times after intravenous administration
Publication date: 25 September 2016 Source:International Journal of Pharmaceutics, Volume 511, Issue 2 Author(s): T. Simon-Yarza, T. Baati, F. Neffati, L. Njim, P. Couvreur, C. Serre, R. Gref, M. Fadhel Najjar, A. Zakhama, P. Horcajada Metal-organic frameworks have shown interesting features for biomedical applications, such as drug delivery and imaging agents. The benchmarked mesoporous iron(III) trimesate MIL-100 MOF nanocarrier combines progressive release of high drug cargoes with absence of visible in vivo toxicity. Although in a previous study pharmacokinetics and biodistribution of MIL-100 nanoparticles were evalua...
Source: International Journal of Pharmaceutics - August 18, 2016 Category: Drugs & Pharmacology Source Type: research

A Design of Experiment approach to predict product and process parameters for a spray dried influenza vaccine
Publication date: 25 September 2016 Source:International Journal of Pharmaceutics, Volume 511, Issue 2 Author(s): Gaurav Kanojia, Geert-Jan Willems, Henderik W. Frijlink, Gideon F.A. Kersten, Peter C. Soema, Jean-Pierre Amorij Spray dried vaccine formulations might be an alternative to traditional lyophilized vaccines. Compared to lyophilization, spray drying is a fast and cheap process extensively used for drying biologicals. The current study provides an approach that utilizes Design of Experiments for spray drying process to stabilize whole inactivated influenza virus (WIV) vaccine. The approach included systematically...
Source: International Journal of Pharmaceutics - August 18, 2016 Category: Drugs & Pharmacology Source Type: research

Drug in adhesive patch of palonosetron: Effect of pressure sensitive adhesive on drug skin permeation and in vitro-in vivo correlation
Publication date: 25 September 2016 Source:International Journal of Pharmaceutics, Volume 511, Issue 2 Author(s): Chao Liu, Mei Hui, Peng Quan, Liang Fang Palonosetron (PAL) is recommended for the prevention of chemotherapy-induced nausea and vomiting. The aim of this study was to develop a long-acting PAL transdermal patch to improve patient compliance. We were particularly concerned about the effect of pressure sensitive adhesives (PSAs) on PAL skin permeability. Formulation factors including PSAs, backing films and drug loadings were investigated in the in vitro skin permeation study using rabbit skin. Fourier transfor...
Source: International Journal of Pharmaceutics - August 18, 2016 Category: Drugs & Pharmacology Source Type: research

Biomaterials based on freeze dried surface-deacetylated chitin nanofibers reinforced with sulfobutyl ether β-cyclodextrin gel in wound dressing applications
Publication date: 25 September 2016 Source:International Journal of Pharmaceutics, Volume 511, Issue 2 Author(s): Ryo Tabuchi, Kazuo Azuma, Ryotaro Izumi, Tsubasa Tanou, Yoshiharu Okamoto, Tomone Nagae, Daisuke Iohara, Kaneto Uekama, Masaki Otagiri, Fumitoshi Hirayama, Shinsuke Ifuku, Makoto Anraku A freeze-dried gel composed of surface-deacetylated chitin nanofibers (SDACNFs), reinforced with an anionic cyclodextrin, sulfobutyl ether β-cyclodextrin (SBE-β-CD) was evaluated for treating wounds in a rat model, and the results were compared with a SDACNFs gel without SBE-β-CD. The incorporation of prednisolon...
Source: International Journal of Pharmaceutics - August 18, 2016 Category: Drugs & Pharmacology Source Type: research

Dual-targeting hybrid peptide-conjugated doxorubicin for drug resistance reversal in breast cancer
In this study, a dual-targeting hybrid peptide HAIYPRHGGCGMPKKKPTPIQLNP (T10-ERK), which is composed of ERK peptide inhibitor MPKKKPTPIQLNP, a thiol spacer (i.e., GGCG) and transferrin receptor (TfR)-binding peptide HAIYPRH, was designed. Then, this thiol-modified hybrid peptide was conjugated to DOXO-EMCH (6-maleimidocaproyl) hydrazone of DOX), forming a novel peptide-DOX conjugate T10-ERK-DOX. The structure and properties of this conjugate were characterized using 1H NMR, mass spectrometry and HPLC. Using MCF-7/ADR cells as an in vitro model system and nude mice bearing MCF-7/ADR xenografts as an in vivo model, the abili...
Source: International Journal of Pharmaceutics - August 18, 2016 Category: Drugs & Pharmacology Source Type: research

Nanoparticle-mediated siRNA delivery assessed in a 3D co-culture model simulating prostate cancer bone metastasis
This study aimed to develop and characterise a 3D in vitro co-culture model to simulate prostate cancer bone metastasis and to assess the ability of the model to investigate nanoparticle-mediated siRNA delivery and gene knockdown. PC3 or LNCaP prostate cancer cells were co-cultured with hFOB 1.19 osteoblast cells in 2D on plastic tissue culture plates and in 3D on collagen scaffolds mimicking the bone microenvironment. To characterise the co-culture model, cell proliferation, enzyme secretion and the utility of two different gene delivery vectors to mediate siRNA uptake and gene knockdown were assessed. Cell proliferation ...
Source: International Journal of Pharmaceutics - August 17, 2016 Category: Drugs & Pharmacology Source Type: research

Controlled drug release from lung-targeted nanocarriers via chemically mediated shell permeabilisation
Publication date: 25 September 2016 Source:International Journal of Pharmaceutics, Volume 511, Issue 2 Author(s): Hanpeng Chen, Arcadia Woods, Ben Forbes, Stuart Jones Nanocarriers can aid therapeutic agent administration to the lung, but controlling drug delivery from these systems after deposition in the airways can be problematic. The aim of this study was to evaluate if chemically mediated shell permeabilisation could help manipulate the rate and extent of nanocarrier drug release. Rifampicin was loaded into lipid shell (loading efficiency 41.0±11.4%, size 50nm) and polymer shell nanocarriers (loading efficienc...
Source: International Journal of Pharmaceutics - August 17, 2016 Category: Drugs & Pharmacology Source Type: research

H2O2-responsive antioxidant polymeric nanoparticles as therapeutic agents for peripheral arterial disease
In this study, we investigated the therapeutic efficacy of PVAX nanoparticles for PAD using a cell culture model and a mouse model of hindlimb ischemia. PVAX nanoparticles significantly enhanced the expression of angiogenic inducers such as vascular endothelial growth factor (VEGF) and platelet endothelial cell adhesion molecule (PECAM)-1 in human umbilical vein endothelial cells (HUVEC). PVAX nanoparticles promoted revascularization and restoration of blood perfusion into ischemic tissues by upregulating angiogenic VEGF and PECAM-1. This work demonstrates that H2O2-responsive PVAX nanoparticles facilitate therapeutic angi...
Source: International Journal of Pharmaceutics - August 17, 2016 Category: Drugs & Pharmacology Source Type: research

Controlled curcumin release via conjugation into PBAE nanogels enhances mitochondrial protection against oxidative stress
Publication date: 25 September 2016 Source:International Journal of Pharmaceutics, Volume 511, Issue 2 Author(s): Prachi Gupta, Carolyn T. Jordan, Mihail I. Mitov, D. Allan Butterfield, J. Zach Hilt, Thomas D. Dziubla Mitochondria are considered to be the “power plants” of the cell, but can also initiate and execute cell death, stimulated by oxidative stress (OS). OS induced mitochondrial dysfunction is characterized by a loss in oxygen consumption and reduced ATP production. Curcumin, as a potential therapeutic, has been explored as a candidate for mitochondrial OS suppression, but rapid metabolism and aqueou...
Source: International Journal of Pharmaceutics - August 17, 2016 Category: Drugs & Pharmacology Source Type: research

Design of spray dried insulin microparticles to bypass deposition in the extrathoracic region and maximize total lung dose
This study evaluated a co-solvent spray drying approach to modulate particle morphology and dose delivery characteristics of engineered powder formulations of insulin microparticles. The binary co-solvent system studied included water as the primary solvent mixed with an organic co-solvent, e.g., ethanol. Factors such as the relative rate of evaporation of each component of a binary co-solvent mixture, and insulin solubility in each component were considered in selecting feedstock compositions. A water-ethanol co-solvent mixture with a composition range considered suitable for modulating particle shell formation during dry...
Source: International Journal of Pharmaceutics - August 17, 2016 Category: Drugs & Pharmacology Source Type: research

Continuous twin screw granulation of controlled release formulations with various HPMC grades
Publication date: 25 September 2016 Source:International Journal of Pharmaceutics, Volume 511, Issue 2 Author(s): V. Vanhoorne, L. Janssens, J. Vercruysse, T. De Beer, J.P. Remon, C. Vervaet HPMC is a popular matrix former to formulate tablets with extended drug release. Tablets with HPMC are preferentially produced by direct compression. However, granulation is often required prior to tableting to overcome poor flowability of the formulation. While continuous twin screw granulation has been extensively evaluated for granulation of immediate release formulations, twin screw granulation of controlled release formulations i...
Source: International Journal of Pharmaceutics - August 17, 2016 Category: Drugs & Pharmacology Source Type: research

Biodegradable brush-type copolymer modified with targeting peptide as a nanoscopic platform for targeting drug delivery to treat castration-resistant prostate cancer
Publication date: 25 September 2016 Source:International Journal of Pharmaceutics, Volume 511, Issue 2 Author(s): Tao Liu, Qianxia Huang Well-defined amphiphilic tumor-targeting brush-type copolymers, poly(oligo(ethylene glycol) monomethyl ether methacrylate-co-G3-C12)-g-poly(ε-caprolactone) (P(OEGMA-co-G3-C12)-g- PCL), were synthesized by the combination of ring-opening polymerization (ROP), reversible addition-fragmentation transfer (RAFT) polymerization and polymer post-functionalization, in which G3-C12 was castration-resistant prostate cancer (CRPC) targeting peptide. The obtained polymers were then employed ...
Source: International Journal of Pharmaceutics - August 12, 2016 Category: Drugs & Pharmacology Source Type: research

Counter-ion complexes for enhanced drug loading in nanocarriers: Proof-of-concept and beyond
Publication date: 25 September 2016 Source:International Journal of Pharmaceutics, Volume 511, Issue 2 Author(s): Nazende Günday Türeli, Akif E. Türeli, Marc Schneider Enhanced drug loading is an important prerequisite of nanomedicines, to reach administration dose while reducing the amount of excipient. Considering biocompatible and biodegradable polymers such as PLGA, pH dependent solubility characteristics along with limited organic solvent solubility of the drug hampers nanoparticle (NP) preparation. To improve loading of such molecules, a method based on using counter ions for complex formation is prop...
Source: International Journal of Pharmaceutics - August 12, 2016 Category: Drugs & Pharmacology Source Type: research